Acarbose: its role in the treatment of diabetes mellitus (original) (raw)
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Acarbose in the treatment of elderly patients with type 2 diabetes
Diabetes Research and Clinical Practice, 2003
To study the effect of acarbose, an a-glucosidase inhibitor, on glycemic control in elderly patients with type 2 diabetes. Methods: Elderly patients with type 2 diabetes treated with diet alone were randomly treated in a double-blind fashion with placebo (n 0/99) or acarbose (n 0/93) for 12 months. Results: After 12 months of therapy, there was a statistically significant difference in the change in glycated haemoglobin (HbA 1c ) ((/0.6%) in the acarbose group versus placebo, as well as in the incremental post-prandial glucose values ((/2.1 mmol h/l) and mean fasting plasma glucose ((/ 0.7 mmol/l). Although there was no effect of acarbose on insulin release, there was a clear effect of acarbose to decrease relative insulin resistance ((/0.8) (HOMA method). In addition, acarbose was generally well tolerated and safe in the elderly; most discontinuations were due to gastrointestinal side effects such as flatulence and diarrhea. There were no
New horizons in diabetes therapy--alpha glucosidase inhibitors
PubMed, 1994
A normal life despite diabetes is only possible when intervention therapy aims at achieving a physiological level of blood glucose and HbA 1c, maintenance of a desirable body weight and serum lipids to avoid hyperinsulinaemia and late diabetes complications and to retard the development of atherosclerosis 1. The first revolution in the treatment of diabetes came with the discovery of insulin in 1921, before which nearly 64% diabetic subjects died prematurely in diabetic coma 2. This was followed by the introduction of oral anti-diabetic suiphonylureas and biguanides about 3 decades ago. The suiphonylureas increase endogenous insulin secretion from the beta cells of the pancreas thus lowering the elevated blood sugar levels through a physiological action of insulin. The basic requirement for suiphonylureas to be effective are functioningbeta cells 3. Biguanides act through a different pathway to produce their hypoglycaemic effect. Several mechanisms have been implicated of which reduction in gastrointestinal glucose obsorption, increased anaerobic glycolysis, inhibition of gluconeogenesis, stimulation of peripheral glucose uptake and increased binding of insulin to its receptor are the most accepted 3. A new concept introduced in the treatment of diabetes mellitus was the postponement of intestinal glucose absorption. This was achieved by the introduction of a-glucosidase inhibitors in the form of acarbose 4,5. Delaying glucose absorption in the gut was attempted first by dietary modification. The nutrient load was spread out into frequent small servings throughout the day. This provided a stable blood glucose and prevented steep rises. This holds good for both insulin dependent and non-insulin dependent diabetics. Complex carbohydrates from starchy foods do not raise blood sugar levels as much as simple ones. Fibre in the food slows down carbohydrate absorption and reduces fasting blood glucose, glycosylated haemoglobin and serum lipid levels. Dietary modification does delay glucose absorption but it does not solve the problem of postprandial hyperglycaemia. This leads to the new pharmacological approach through alteration of the activity of intestinal a-glucosidase by using specific inhibitors 6. Acarbose, isolated from fermentation of actinoptanes strains, is a pseudotetrasaccharide of microbial origin 7. It is a competitive and reversible inhibitor of intestinal aglucosidase activity 8. a-glucosidases are located in the luminal brush border formed by enterocytes of the small gut. Since carbohydrates are taken up in the form of monosaccharides only in the intestine, the disaccharides and polysaccharides are broken down by glucosidases before they can be absorbed 9. In this process cc-glucosidase inhibitors delay carbohydrate digestion leading to delayed glucose absorption. Glucose, fructose and sorbitol which are directly absorbed and un digestable carbohydrates as cellulose, are not affected by the drug. Thus the efficacy of a-glucosidase inhibitors depends on the carbohydrate composition of the meals. Studies conducted with acarbose on non-insulin-dependent diabetic patients demonstrated an improved metabolic control regardless of whether being administered in addition to oral hypoglycaemic agents or to a diet alone 10,11. The most significant finding was a reduction in the post-prandial blood glucose concentration. Evidence was also had for a reduction in serum insulin levels 12. Acarbose does not lead to malabsorption of carbohydrates. A diet rich in poorly digestable complex carbohydrates causing an intestinal load will result in bacterial fermentation which can cause flatulence, distension and diarrhoea. Due to an effective assimilation in the large bowel no faecal loss of calories takes place 9. Studies have been conducted on IDDM patients by adding acarbose to their insulin regime. Post-prandial blood glucose concentrations are reduced, smoother diurnal blood glucose profiles were achieved and in some cases the daily insulin requirement was reduced 13. The
The Effect of Acarbose on Insulin Sensitivity in Subjects With Impaired Glucose Tolerance
Diabetes Care, 1996
OBJECTIVE To study the effect of acarbose, an α-glucosidase inhibitor, on postprandial plasma glucose and insulin and insulin sensitivity in subjects with impaired glucose tolerance (IGT). RESEARCH DESIGN AND METHODS Subjects with IGT were randomly treated in a double-blind fashion with placebo (n = 10) or acarbose (n = 8) at 100 mg t.i.d. for 4 months. All subjects were submitted before randomization and at the end of the study to a standardized breakfast and a 12-h daytime plasma glucose and plasma insulin profile, and insulin sensitivity was measured as steady-state plasma glucose (SSPG) using the insulin suppression test. RESULTS While placebo had no effect on postprandial plasma glucose and plasma insulin incremental area under the curve (AUC) (3.03 ± 0.5 vs. 3.76 ± 0.6 mmol·h−1 · l−1, P = NS; 1,488 ± 229 vs. 1,609 ± 253 pmol · h−1 · l−1, P = NS), acarbose resulted in a significant reduction for both glucose (1.44 ± 0.3 vs. 4.45 ± 0.9 mmol · h−1 · l−1, P = 0.002) and insulin (6...
Clinical Drug Investigation, 2013
Background and Objectives The burden of type 2 diabetes mellitus is growing rapidly, particularly in the Asia-Pacific region. The aim of this international, largescale, observational study was to investigate the efficacy and tolerability of the antidiabetic agent acarbose as add-on or monotherapy in a range of patients with type 2 diabetes, including those with cardiovascular morbidities. The majority of practices were included from high-burden regions (predominantly those in the Asia-Pacific region). Methods This was an observational study conducted in 15 countries/regions. Adults with pre-treated or untreated type 2 diabetes prescribed acarbose as add-on or monotherapy were eligible. Two-hour postprandial blood glucose (2-h PPG), glycosylated haemoglobin (HbA 1c) and fasting blood glucose (FBG) were measured over a 3-month observation period. Results A total of 15,034 patients were valid for the efficacy analysis and 15,661 for the safety analysis (mean age was 57.6 years and 92.6 % of patients were Asian). Mean (SD) 2-h PPG decreased by-71.9 (62.3) mg/dL, to 170.2 (46.5) mg/dL at final visit (after 12.8 [4.1] weeks). Mean HbA 1c decreased by-1.1 % (1.3) to 7.2 % (1.1) and mean FBG decreased by-33.0 (43.3) mg/dL to 124.8 (30.5) mg/dL. Acarbose was effective regardless of the presence of cardiovascular co-morbidities or diabetic complications. The efficacy of acarbose was rated 'very good' or 'good' in 85.5 % of patients, and tolerability as 'very good' or 'good' in 84.9 % of patients. Drug-related adverse events, mainly gastrointestinal, were reported in 490/15,661 patients (3.13 %). Conclusion The results of this observational study support the notion that acarbose is effective, safe and well tolerated in a large cohort of Asian patients with type 2 diabetes. On behalf of the GlucoVIP Investigators. The GlucoVIP investigators are given in the Appendix.
Long-term efficacy and tolerability of acarbose treatment in patients with type 2 diabetes mellitus
Clinical drug …, 2005
long-term acarbose therapy in type 2 diabetic patients. Study design: In this double-blind, single-centre group comparison, patients were randomised to receive either acarbose or matching placebo, in addition to their regular antidiabetic therapy, over a period of 78 weeks. Eligibility for inclusion in the efficacy evaluation included a study duration of ≥510 days. Methods: The primary efficacy parameter was the change in glycosylated haemoglobin (HbA1) from baseline to end of study. Secondary variables included changes in blood glucose and lipid parameters, as well as signs of retinopathy and nephropathy. Patients: A total of 139 patients were assessed for safety and 88 patients (44 in each treatment group) were included in the efficacy analysis. Patients were generally overweight and the majority had previously been treated with sulphonylureas. Results: Acarbose significantly improved fasting and 1-hour postprandial blood glucose levels compared with placebo (p = 0.039 and 0.009), and improvements in HbA1 with acarbose versus placebo fell just short of significance (p = 0.057). There were no differences between treatments in changes in microvascular complications, but blood pressure improved with acarbose treatment. Two patients in the acarbose group experienced elevated liver enzyme levels. Generally, acarbose had a good safety profile and was well tolerated. Conclusion: Long-term treatment with acarbose was safe and efficacious in patients with type 2 diabetes mellitus that was insufficiently controlled by other oral antidiabetics. 18. Lam KSL, Tiu SC, Tsang MW, et al. Acarbose in NIDDM
Archives of Medical Science, 2012
Post-prandial hyperglycemia still remains a problem in the management of type 2 diabetes mellitus. Of all available anti-diabetic drugs, α-glucosidase inhibitors seem to be the most effective in reducing post-prandial hyperglycemia. We conducted a review analyzing the clinical efficacy and safety of α-glucosidase inhibitors, both alone and in combination with other anti-diabetic drugs, with respect to glycemic control, inflammation and atherosclerosis. α-Glucosidase inhibitors proved to be effective and safe both in monotherapy and as an addon to other anti-diabetic drugs. Compared to miglitol and voglibose, acarbose seems to have some additive effects such as stabling carotid plaques, and reducing inflammation. Acarbose also proved to reverse impaired glucose tolerance to normal glucose tolerance.
Protocols, 1996
Analysis 1.1. Comparison 1 Acarbose versus placebo, Outcome 1 Incidence of type 2 diabetes mellitus.. .. .. Analysis 1.2. Comparison 1 Acarbose versus placebo, Outcome 2 Occurrence of death (total).. .. .. .. . Analysis 1.3. Comparison 1 Acarbose versus placebo, Outcome 3 Occurrence of cardiovascular death.. .. .. . Analysis 1.4. Comparison 1 Acarbose versus placebo, Outcome 4 Occurrence of cardiovascular disease (any).. .. Analysis 1.5. Comparison 1 Acarbose versus placebo, Outcome 5 Occurrence of myocardial infarctions.. .. .. Analysis 1.6. Comparison 1 Acarbose versus placebo, Outcome 6 Occurrence of angina pectoris.. .. .. .. Analysis 1.7. Comparison 1 Acarbose versus placebo, Outcome 7 Occurrence of revascularisation procedures.. .. Analysis 1.8. Comparison 1 Acarbose versus placebo, Outcome 8 Occurrence of congestive heart failure.. .. .. Analysis 1.9. Comparison 1 Acarbose versus placebo, Outcome 9 Occurrence of cerebrovascular events.. .. .. Analysis 1.10. Comparison 1 Acarbose versus placebo, Outcome 10 Occurrence of peripheral vascular events.. .. Analysis 1.11. Comparison 1 Acarbose versus placebo, Outcome 11 Change in glycated haemoglobin (%).. .. . Analysis 1.12. Comparison 1 Acarbose versus placebo, Outcome 12 Change in fasting blood glucose (mmol/l).. . Analysis 1.13. Comparison 1 Acarbose versus placebo, Outcome 13 Change in post-load blood glucose (mmol/l).. Analysis 1.14. Comparison 1 Acarbose versus placebo, Outcome 14 Change in total cholesterol (mmol/l).. .. . Analysis 1.15. Comparison 1 Acarbose versus placebo, Outcome 15 Change in HDL-cholesterol (mmol/l).. .. . Analysis 1.16. Comparison 1 Acarbose versus placebo, Outcome 16 Change in LDL-cholesterol (mmol/l).. .. . Analysis 1.17. Comparison 1 Acarbose versus placebo, Outcome 17 Change in triglycerides (mmol/l).. .. .. Analysis 1.18. Comparison 1 Acarbose versus placebo, Outcome 18 Change in fasting insulin levels (pmol/l).. .. Analysis 1.19. Comparison 1 Acarbose versus placebo, Outcome 19 Change in post-load insulin levels (pmol/l).. . Analysis 1.20. Comparison 1 Acarbose versus placebo, Outcome 20 Change in body weight (Kg).. .. .. .. Analysis 1.21. Comparison 1 Acarbose versus placebo, Outcome 21 Change in body mass index (Kg/m2).. .. . Analysis 1.22. Comparison 1 Acarbose versus placebo, Outcome 22 Change in diastolic blood pressure (mmHg).. Analysis 1.23. Comparison 1 Acarbose versus placebo, Outcome 23 Change in systolic blood pressure (mmHg).. . Analysis 1.24. Comparison 1 Acarbose versus placebo, Outcome 24 Occurrence of side effects (total).. .. .. . Analysis 1.25. Comparison 1 Acarbose versus placebo, Outcome 25 Occurrence of gastro-intestinal side-effects.. . Analysis 2.1. Comparison 2 Acarbose versus metformin, Outcome 1 Incidence of type 2 diabetes mellitus.. .. . Analysis 2.2. Comparison 2 Acarbose versus metformin, Outcome 2 Change in fasting blood glucose (mmol/l).. . Analysis 2.3. Comparison 2 Acarbose versus metformin, Outcome 3 Change in post-load blood glucose (mmol/l).. Analysis 2.4. Comparison 2 Acarbose versus metformin, Outcome 4 Change in total cholesterol (mmol/l).. .. . Analysis 2.5. Comparison 2 Acarbose versus metformin, Outcome 5 Change in triglycerides (mmol/l).. .. .. Analysis 2.6. Comparison 2 Acarbose versus metformin, Outcome 6 Change in body mass index (Kg/m2).. .. . Analysis 2.7. Comparison 2 Acarbose versus metformin, Outcome 7 Change in diastolic blood pressure (mmHg).. Analysis 2.8. Comparison 2 Acarbose versus metformin, Outcome 8 Change in systolic blood pressure (mmHg).. . Analysis 3.1. Comparison 3 Acarbose versus diet and exercise, Outcome 1 Incidence of type 2 diabetes mellitus.. . Analysis 3.2. Comparison 3 Acarbose versus diet and exercise, Outcome 2 Change in fasting blood glucose (mmol/l). Analysis 3.3. Comparison 3 Acarbose versus diet and exercise, Outcome 3 Change in post-load blood glucose (mmol/l). Analysis 3.4. Comparison 3 Acarbose versus diet and exercise, Outcome 4 Change in total cholesterol (mmol/l).. .
Alpha-glucosidase inhibitors for type 2 diabetes mellitus
Reviews, 1996
BACKGROUND: Alpha-glucosidase inhibitors such as acarbose or miglitol, have the potential to improve glycemic control in type 2 diabetes mellitus. The true value of these agents, especially in relation to diabetes related mortality and morbidity, has never been investigated in a systematic literature review and meta-analysis. OBJECTIVES: To assess the effects of alpha-glucosidase inhibitors s in patients with type 2
Indian Journal of Endocrinology and Metabolism, 2013
S674 inTRoducTion Diabetes is among the most challenging health problems of 21 st century. According to prevalence estimation of the International Diabetes Federation, 366 million people had diabetes in 2011; by 2030 this may rise to 552 million. [1] It has been estimated that 20% of global burden resides in South Eastern Asia Region, which will be tripled to 228 million by the year 2025 from the current 84 million. [2] India along with China will account for nearly a third of the estimated 300 million adult diabetics by the year 2025. [3] Prospective randomized controlled studies such as the Diabetes Prevention Program (DPP) in the USA, [4] the Finnish Diabetes Prevention Study [5] (DPS), the Da Qing impaired glucose tolerance (IGT) and Diabetes Study in China [6] and the Malmo study in Sweden [7] have shown that lifestyle modification involving diet and enhanced physical